CRA-026440 hydrochloride

Modify Date: 2025-08-22 20:56:20

CRA-026440 hydrochloride Structure
CRA-026440 hydrochloride structure
Common Name CRA-026440 hydrochloride
CAS Number 847459-98-7 Molecular Weight 456.92
Density N/A Boiling Point N/A
Molecular Formula C23H25ClN4O4 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of CRA-026440 hydrochloride


CRA-026440 hydrochloride is a potent, broad-spectrum HDAC (HDAC) inhibitor. The Ki values against recombinant HDAC isoenzymes HDAC1, HDAC2, HDAC3, HDAC6, HDAC8, and HDAC10 are 4 nM, 14 nM, 11 nM, 15 nM, 7 nM, and 20 nM respectively. CRA-026440 hydrochloride shows antitumor and antiangiogenic activities[1].

 Names

Name CRA-026440 hydrochloride

 CRA-026440 hydrochloride Biological Activity

Description CRA-026440 hydrochloride is a potent, broad-spectrum HDAC (HDAC) inhibitor. The Ki values against recombinant HDAC isoenzymes HDAC1, HDAC2, HDAC3, HDAC6, HDAC8, and HDAC10 are 4 nM, 14 nM, 11 nM, 15 nM, 7 nM, and 20 nM respectively. CRA-026440 hydrochloride shows antitumor and antiangiogenic activities[1].
Related Catalog
Target

HDAC1:4 nM (IC50)

HDAC2:14 nM (IC50)

HDAC3/SMRT:11 nM (IC50)

HDAC6:15 nM (IC50)

HDAC8:7 nM (IC50)

HDAC10:20 nM (IC50)

In Vitro CRA-026440 hydrochloride 对 HUVEC 内皮细胞具有抗增殖作用,GI50 值为 1.41 μM[1]。 CRA-026440 hydrochloride(0.1-10 μM;18 小时)导致乙酰化组蛋白和乙酰化微管蛋白的积累,从而抑制肿瘤细胞生长并诱导细胞凋亡[1]。 CRA-026440 hydrochloride(0.1-10 μM;5 天)以剂量依赖性方式抑制离体血管生成[1]。 Western Blot Analysis[1] Cell Line: HCT116 cells Concentration: 0.1 μM, 0.5 μM, 1 μM, 5 μM, 10 μM Incubation Time: 18 hours Result: Resulted in the accumulation of both acetylated histones and acetylated tubulin. Induced expression of the cyclin-dependent kinase inhibitor p21Cip1/WAF1.
In Vivo CRA-026440 hydrochloride(100 mg/kg;静脉注射;每天;连续三天)导致携带 HCT116 或 U937 人肿瘤异种移植物的小鼠肿瘤生长显着减少[1]。 Animal Model: HCT-116 tumor-bearing nude mice[1] Dosage: 100 mg/kg Administration: i.v.; daily; for three consecutive days Result: Resulted in a statistically significant reduction in tumor growth.
References

[1]. [1]Cao ZA, et al. CRA-026440: a potent, broad-spectrum, hydroxamic histone deacetylase inhibitor with antiproliferative and antiangiogenic activity in vitro and in vivo. Mol Cancer Ther. 2006 Jul;5(7):1693-701.  

 Chemical & Physical Properties

Molecular Formula C23H25ClN4O4
Molecular Weight 456.92
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